IP Library › Granted Patent US 8,592,398
Granted Patent B2
US 8,592,398 · App. 13/327,128 · Granted Nov 26, 2013

2-amino-4-arylthiazole compounds as TRPA1 antagonists

Inventors: Sukeerthi Kumar (Navi Mumbai, IN); Abraham Thomas (Navi Mumbai, IN); Sachin Sundarlal Chaudhari (Navi Mumbai, IN); Bipin Parsottam Kansagra (Ahmedabad, IN); Venkata Ramana Yemireddy (Maharashtra, IN); Neelima Khairatkar-Joshi (Maharashtra, IN); Indranil Mukhopadhyay (Maharashtra, IN); Girish Gudi (Mumbai, IN)
Assignee: Glenmark Pharmaceuticals, S.A.
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,592,398
App. No.
13/327,128
Granted
Nov 26, 2013
Kind
B2
Abstract

The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.

Claims (30)

1. A compound selected from:

[2{[(1,3-Dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl) acetyl]imino}-4-[3-fluoro-4-(trifluoromethyl)phenyl]-1,3-thiazol-3(2H)-yl]methyl dihydrogen phosphate;

Disodium[2-{[(1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl]imino}-4-[3-fluoro-4-(trifluoromethyl)phenyl]-1,3-thiazol-3(2H)-yl]methyl phosphate;

[4-[2,4-Difluoro-3-(trifluoromethyl)phenyl]-2-{[(1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl]imino}-1,3-thiazol-3(2H)-yl]methyl dihydrogen phosphate;

Disodium[4-[2,4-difluoro-3-(trifluoromethyl)phenyl]-2-{[(1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl]imino}-1,3-thiazol-3(2H)-yl]methyl phosphate;

4-(2,4-Difluoro-3-(trifluoromethyl)phenyl)-2-((2-(1,3,6-trimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl)imino)thiazol-3(2H)-yl)methyl dihydrogen phosphate;

Disodium (4-(2,4-difluoro-3-(trifluoromethyl)phenyl)-2-((2-(1,3,6-trimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl)imino)thiazol-3(2H)-yl)methyl phosphate;

[2-{[(6-ethyl-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl]imino}-4-[3-fluoro-4-(trifluoromethyl)phenyl]-1,3-thiazol-3(2H)-yl]methyl dihydrogen phosphate;

Disodium [2-{[(6-ethyl-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetyl]imino}-4-[3-fluoro-4-(trifluoromethyl)phenyl]-1,3-thiazol-3(2H)-yl]methyl phosphate;

[4-[3-Chloro-4-(trifluoromethoxy)phenyl]-2-{[(1,3,6-trimethyl-2,4-dioxo-1,2,3,4-tetrahydrofuro[2,3-d]pyrimidin-5-yl)acetyl]imino}-1,3-thiazol-3(2H)-yl]methyl dihydrogen phosphate;

Disodium [4-[3-chloro-4-(trifluoromethoxy)phenyl]-2-{[(1,3,6-trimethyl-2,4-dioxo-1,2,3,4-tetrahydrofuro [2,3-d] pyrimidin-5-yl)acetyl]imino}-1,3-thiazol-3(2H)-yl]methyl phosphate:

4-[2,3-Difluoro-4-(trifluoromethyl)phenyl]-2-{[(1,3,6-trimethyl-2,4-dioxo-1,2,3,4-tetrahydrofuro[2,3-d]pyrimidin-5-yl)acetyl]imino}-1,3-thiazol-3(2H)-yl]methyl dihydrogen phosphate;

4-(2,4-Difluoro-3-(trifluoromethyl)phenyl)-2-((2-(2,5,7-trimethyl-4,6-dioxo-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-3-yl)acetyl)imino)thiazol-3(2H)-yl)methyl dihydrogen phosphate;

Disodium-(4-(2,4-difluoro-3-(trifluoromethyl)phenyl)-2-((2-(2,5,7-trimethyl-4,6-dioxo-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-3-yl)acetyl)imino)thiazol-3(2H)-yl)methyl phosphate;

[4-[2,3-Difluoro-4-(trifluoromethyl)phenyl]-2-{[(5,7-dimethyl-4,6-dioxo-4,5,6,7-tetrahydro[1,2]thiazolo[5,4-d]pyrimidin-3-yl)acetyl]imino}-1,3-thiazol-3(2H)-yl]methyl dihydrogen phosphate;

Disodium -(4-(2,3-difluoro-4-(trifluoromethyl)phenyl)-2-((2-(5,7-dimethyl-4,6-dioxo-4,5,6,7-tetrahydroisothiazolo[5,4-d]pyrimidin-3-yl)acetyl)imino)thiazol-3(2H)-yl)methyl phosphate.

or a pharmaceutically acceptable salt thereof.

2. The compound according to claim 1 having structure

or a pharmaceutically acceptable salt thereof

3. The compound according to claim 1 having structure

or a pharmaceutically acceptable salt thereof.

4. The compound according to claim 1 having structure

or a pharmaceutically acceptable salt thereof.

5. The compound according to claim 1 having structure

or a pharmaceutically acceptable salt thereof.

6. The compound according to claim 1 having structure

or a pharmaceutically acceptable salt thereof.

7. The compound according to claim 1 having structure

or a pharmaceutically acceptable salt thereof.

8. A pharmaceutical composition comprising one or more compounds of claim 1 , and one or more pharmaceutically acceptable excipients, carriers, diluents or mixture thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 24, 2013
From: KUMAR, SUKEERTHI; THOMAS, ABRAHAM; CHAUDHARI, SACHIN SUNDARLAL; KANSAGRA, BIPIN PARSOTTAM; YEMIREDDY, VENKATA RAMANA; KHAIRATKAR-JOSHI, NEELIMA; MUKHOPADHYAY, INDRANIL; GUDI, GIRISH
To: GLENMARK PHARMACEUTICALS, S.A.
Reel/Frame 030482/0349 →
Priority Claims (4)
IN 3451/MUM/2010 · Dec 20, 2010 · national
IN 748/MUM/2011 · Mar 16, 2011 · national
IN 1569/MUM/2011 · May 25, 2011 · national
IN 2741/MUM/2011 · Sep 28, 2011 · national
Continuity (5)
Provisional Application 61428327 · Dec 30, 2010
Provisional Application 61466535 · Mar 23, 2011
Provisional Application 61495002 · Jun 9, 2011
Provisional Application 61552076 · Oct 27, 2011
Related Publication 20120157411A1 · Jun 21, 2012